Cellular and Molecular Life Sciences CMLS

, Volume 62, Issue 16, pp 1839-1849

First online:

Cell-penetrating peptides: tools for intracellular delivery of therapeutics

  • S. DeshayesAffiliated withCRBM-CNRS FRE 2593
  • , M. C. MorrisAffiliated withCRBM-CNRS FRE 2593
  • , G. DivitaAffiliated withCRBM-CNRS FRE 2593
  • , F. HeitzAffiliated withCRBM-CNRS FRE 2593 Email author 

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The main problem of therapeutic efficiency lies in the crossing of cellular membranes. Therefore, significant effort is being made to develop agents which can cross these barriers and deliver therapeutic agents into cellular compartments. In recent years, a large amount of data on the use of peptides as delivery agents has accumulated. Several groups have published the first positive results using peptides for the delivery of therapeutic agents in relevant animal models. These peptides, called cell-penetrating peptides (CPPs), are short peptides (fewer than 30 residues) with a net positive charge and acting in a receptor- and energy-independent manner. Here, we give an extensive review of peptide-mediated delivery systems and discuss their applications, with particular focus on the mechanisms leading to cellular internalization.

Key words.

Cell-penetrating peptides mechanisms of membrane translocation conformations pore-like structure peptide-mediated delivery